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Azelaic Acid


General


Pronunciation

(a zeh LAY ik AS id)


Brand Names: U.S.

  • Azelex
  • Finacea

Indications


Use: Labeled Indications

Acne vulgaris (cream): Treatment of mild to moderate inflammatory acne vulgaris.

Rosacea (foam, gel): Treatment of inflammatory papules and pustules of mild to moderate rosacea.

Limitations of use: Efficacy for treatment of erythema in rosacea in the absence of papules and pustules has not been evaluated.


Contraindications


Cream: Hypersensitivity to azelaic acid or any component of the formulation

Foam, gel: There are no contraindications listed in the manufacturer 's labeling


Dosing and Administration


Dosing: Adult

Acne vulgaris: Topical: Cream 20%: Apply a thin film to the affected area(s) twice daily, in the morning and evening; may reduce to once daily if persistent skin irritation occurs. Improvement in condition is usually seen within 4 weeks.

Rosacea: Topical: Gel 15% and foam 15%: Apply a thin layer to the affected area(s) of the face twice daily, in the morning and evening; reassess if no improvement after 12 weeks of therapy.


Dosing: Geriatric

Refer to adult dosing.


Dosing: Pediatric

Acne vulgaris: Children ≥12 years and Adolescents: Refer to adult dosing.


Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturers labeling. However, dosage adjustment unlikely due to low systemic absorption.


Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturers labeling. However, dosage adjustment unlikely due to low systemic absorption.


Administration

Apply a thin film and gently massage into to clean, dry skin; wash hands following application. Avoid the use of occlusive dressings or wrappings. For foam and gel formulations, cosmetics may be applied after the foam or gel has dried. Use only mild soaps or soapless cleansing lotion for facial cleansing. Not intended for intravaginal, ophthalmic, or oral use.

Foam: Shake well before use.


Dietary Considerations

Gel: Foods and beverages that might provoke erythema, flushing, and blushing, such as spicy food, alcoholic beverages, and thermally hot drinks (including hot coffee and tea), should be avoided.


Storage

Store at 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F); do not freeze. Store cream on its side.

Foam: Store at 25 ‚ °C (77 ‚ °F); excursions are permitted between 15 ‚ °C and 30 ‚ °C (59 ‚ °F and 86 ‚ °F). Flammable; avoid fire, flame, or smoking during and immediately following application. Contents under pressure. Do not puncture or incinerate. Do not expose to heat or store at temperatures above 49 ‚ °C (120 ‚ °F). Discard 8 weeks after opening.


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Cream, External:

Azelex: 20% (30 g, 50 g)

Foam, External:

Finacea: 15% (50 g) [contains benzoic acid, cetostearyl alcohol, polysorbate 80, propylene glycol]

Gel, External:

Finacea: 15% (50 g) [contains benzoic acid, disodium edta, polysorbate 80, propylene glycol]


Drug Interactions

There are no known significant interactions.


Adverse Reactions


>10%: Dermatologic: Burning sensation of skin ( ≤16%), stinging of skin ( ≤16%), tingling of skin ( ≤16%)

1% to 10%:

Dermatologic: Pruritus (1% to 6%), erythema ( ≤2%), skin irritation ( ≤2%), acne (gel: ≤1%), contact dermatitis ( ≤1%), desquamation ( ≤1%), xeroderma ( ≤1%), xerosis ( ≤1%)

Local: Application site pain (6%), application site pruritus (3%)

<1% (Limited to important or life-threatening): Edema, exacerbation of asthma, exacerbation of herpes labialis, hypersensitivity reaction, hypertrichosis, hypopigmentation, iridocyclitis, vitiligo


Warnings/Precautions


Concerns related to adverse effects:

- Hypersensitivity: Hypersensitivity reactions have been reported; discontinue use if signs/symptoms occur.

- Hypopigmentation: A few cases of hypopigmentation after use have been reported; monitor for changes in skin color, especially in patients with dark complexions.

- Skin irritation: Skin irritation (eg, pruritus, burning, stinging) may occur, usually during the first weeks of therapy. Discontinue use if severe skin irritation or sensitivity occurs.

Dosage form specific issues:

- Foam: Contains flammable propellants. Avoid fire, flame and smoking during and immediately following use.

- Gel: Reassess use if no improvement is seen after 12 weeks of therapy.

- Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer 's labeling.

Other warnings/precautions:

- Appropriate use: For external use only; not for oral, ophthalmic, or vaginal use; avoid contact with the eyes, mouth, and other mucous membranes. Use of occlusive dressings or wrappings should be avoided.


Pregnancy Risk Factor

B


Pregnancy Considerations

Adverse events have been observed in animal reproduction studies following oral administration. The amount of azelaic acid available systemically following topical administration is minimal (<4%).


Actions


Pharmacology

Azelaic acid is a dietary constituent normally found in whole grain cereals; can be formed endogenously. Exact mechanism is not known. In vitro, azelaic acid possesses antimicrobial activity against Propionibacterium acnes and Staphylococcus epidermidis. May decrease microcomedo formation.


Absorption

Cream: ~3% to 5% penetrates stratum corneum; up to 10% found in epidermis and dermis; 4% systemic


Metabolism

Negligible after topical application; some beta-oxidation to shorter chain dicarboxylic acids


Excretion

Urine (primarily as unchanged drug)


Onset of Action

Cream: Within 4 weeks


Half-Life Elimination

Topical: Healthy subjects: 12 hours


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience itching, burning, or stinging. Have patient report immediately to prescriber severe skin irritation, peeling, or skin discoloration (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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